PTK6 (BRK)
PTK6, also called breast tumour kinase, is over-expressed in most breast cancers and is one of the off-targets of dasatinib; drugs made specifically against it are still experimental.
Overview
Protein tyrosine kinase 6, or breast tumour kinase (BRK), is a distant relative of the SRC family that is normally found in differentiating gut and skin epithelium but is over-expressed in the majority of breast cancers and in some colon, prostate and ovarian tumours, where it promotes proliferation, survival and migration through STAT3 and AKT. It appears in ChEMBL as a target because approved multi-kinase inhibitors, dasatinib among them, inhibit it; selective PTK6 inhibitors and degraders are in preclinical development, including for HER2-positive and triple-negative breast cancer.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · PTK6, also called breast tumour kinase, is over-expressed in most breast cancers and is one of the off-targets of dasatinib; drugs made specifically against it are still experimental.
- 1 · What it is
PTK6, also called breast tumour kinase, is over-expressed in most breast cancers and is one of the off-targets of dasatinib; drugs made specifically against it are still experimental.
- 2 · What goes wrong in cancer
An intracellular non-receptor tyrosine kinase lacking a membrane anchor; in tumours it phosphorylates STAT3, paxillin and Sam68 and cooperates with HER2 and EGFR signalling.
- 3 · How drugs use it
No product in this corpus aims at PTK6 (BRK) yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
External identifiers
Biology
An intracellular non-receptor tyrosine kinase lacking a membrane anchor; in tumours it phosphorylates STAT3, paxillin and Sam68 and cooperates with HER2 and EGFR signalling.
- Differentiated intestinal and skin epithelium
- Most breast cancers; some colon, prostate and ovarian cancers
Latest papers
topQuery for this target: (TITLE:"PTK6" OR ABSTRACT:"PTK6" OR TITLE:"BRK" OR ABSTRACT:"BRK") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about PTK6 (BRK), not a curated reading list.
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